Composition
Each capsule contains Fluconazole 50 mg.
Pharmacology
Fluconazole is a triazole antifungal drug which acts by inhibition of the ergosterol component of the fungal cell membrane. It is active against a broad spectrum of fungal pathogens and is available for oral use. Following oral administration, absorption is rapid and extensive (>90%). Bioavailability is the same in the fasting and fed states. The bioavailability of Fluconazole is unaffected by gastric pH. The plasma half life is approximately 30h. The plasma protein binding of Fluconazole is low, at 11% and the drug is widely distributed throughout the body. Most of the dose of Fluconazole is excreted unchanged in the urine, the reminder of the dose being eliminated in the urine as metabolites.
Indication
Fluconazole is indicated in the treatment of acute or recurrent vaginal candidiasis, mucosal candidiasis (as oropharyngeal candidiasis, oesophagitis, candiduria), systemic candidiasis and cryptococcal infections (including meningitis).
Dosage & Administration
Adults
Since oral absorption is rapid and almost complete, the daily dose of Fluconazole is the same for oral and intravenous administration.
Oropharyngeal Candidiasis: The recommended dosage of fluconazole for oropharyngeal candidiasis is 200 mg on the first day, followed by 100 mg once daily for 7-14 days.
Esophageal Candidiasis: The recommended dosage of fluconazole for esophageal candidiasis is 200 mg on the first day, followed by 100 mg once daily for 2-3 weeks.
Systemic Candidiasis and Cryptococcal Meningitis: 400 mg daily followed by 200 mg once daily. The recommended duration of treatment for initial therapy of cryptococcal meningitis is 10 to 12 weeks.
Acute or recurrent vaginal candidiasis: Single dose of 150 mg.
Urinary Tract Infections and Peritonitis: 50 to 200 mg once daily.
Prophylaxis in Patients Undergoing Bone Marrow Transplantation: 400 mg once daily.
Children
Oropharyngeal Candidiasis: The recommended dosage of Fluconazole for oropharyngeal candidiasis in children is 6 mg/kg on the first day, followed by 3 mg/kg once daily. Treatment should be administered for at least 2 weeks to decrease the likelihood of relapse.
Esophageal Candidiasis: Recommended dosage of Fluconazole in children is 6 mg/kg on the first day, followed by 3 mg/kg once daily.
Cryptococcal meningitis: Initial therapy should be started with 6 to 12 mg/kg daily. Doses up to 12 mg/kg/day may be used for three weeks and treatment for initial therapy of cryptococcal meningitis is 10 to 12 weeks.
Contraindication
Fluconazole is contraindicated to patients hypersensitive to this drug and in advanced liver disease.
Precaution
Caution should be taken in renal impairment, pregnancy and breast feeding and in raised liver enzymes. The use of Fluconazole in lactating mothers is not recommended.
Side Effects
Nausea, abdominal discomfort, diarrhoea and flatulence, occasionally abnormalities of liver enzymes; rarely rash; angioedema and anaphylaxis reported.
Use in Pregnancy & Lactation
Fluconazole adverse fetal effects have been seen in animals only at dose levels associated with maternal toxicity. These levels are many times in excess of those recommended for therapeutic use. There has been little use during human pregnancy. Accordingly, fuconazole should not be used in pregnancy or in women of child bearing potential unless adequate contraception is employed.
Drug Interaction
Rifampicin reduces plasma concentration of Fluconazole. Effects of nicoumalone, phenytoin and warfarin are enhanced. Plasma concentrations of sulphonylureas & theophyline are possibly increased.
Storage
Store below 300C. Protect from light & moisture. Remaining reconstituted suspension should not be used after 7 days. If it is kept under freezing temperature (20C – 80C), it can be used for 14 days. Keep out of the reach of children.
Packaging
Box containing 20 capsules in blister pack.
